WO2002008203A3 - 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by vla-4 - Google Patents

3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by vla-4 Download PDF

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Publication number
WO2002008203A3
WO2002008203A3 PCT/US2001/023097 US0123097W WO0208203A3 WO 2002008203 A3 WO2002008203 A3 WO 2002008203A3 US 0123097 W US0123097 W US 0123097W WO 0208203 A3 WO0208203 A3 WO 0208203A3
Authority
WO
WIPO (PCT)
Prior art keywords
vla
heteroaryl
leukocyte adhesion
inhibitors
adhesion mediated
Prior art date
Application number
PCT/US2001/023097
Other languages
French (fr)
Other versions
WO2002008203A2 (en
Inventor
Andrei W Konradi
Michael A Pleiss
Eugene D Thorsett
Susan Ashwell
Gregory S Welmaker
Anthony Kreft
Dimitrios Sarantakis
Darren B Dressen
Francine S Grant
Christopher Semko
Ying-Zi Xu
Frank Stappenbeck
Original Assignee
Elan Pharm Inc
American Home Prod
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Elan Pharm Inc, American Home Prod filed Critical Elan Pharm Inc
Priority to AU2001277960A priority Critical patent/AU2001277960A1/en
Publication of WO2002008203A2 publication Critical patent/WO2002008203A2/en
Publication of WO2002008203A3 publication Critical patent/WO2002008203A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
PCT/US2001/023097 2000-07-21 2001-07-20 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by vla-4 WO2002008203A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001277960A AU2001277960A1 (en) 2000-07-21 2001-07-20 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by vla-4

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22013100P 2000-07-21 2000-07-21
US60/220,131 2000-07-21

Publications (2)

Publication Number Publication Date
WO2002008203A2 WO2002008203A2 (en) 2002-01-31
WO2002008203A3 true WO2002008203A3 (en) 2002-05-23

Family

ID=22822196

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/023097 WO2002008203A2 (en) 2000-07-21 2001-07-20 3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by vla-4

Country Status (3)

Country Link
US (3) US6794506B2 (en)
AU (1) AU2001277960A1 (en)
WO (1) WO2002008203A2 (en)

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US6479492B1 (en) * 1999-01-22 2002-11-12 Elan Pharmaceuticals, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
MY162179A (en) * 2004-04-01 2017-05-31 Elan Pharm Inc Steroid sparing agents and methods of using same
WO2005111020A2 (en) * 2004-04-30 2005-11-24 Elan Pharmaceuticals, Inc. Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by vla-4
BRPI0616643A2 (en) 2005-09-29 2011-06-28 Elan Pharm Inc carbamate compounds that inhibit vla-4 mediated leukocyte adhesion
AU2006297220B8 (en) * 2005-09-29 2013-01-31 Elan Pharmaceuticals, Inc. Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4
EP1996559A1 (en) * 2006-02-27 2008-12-03 Elan Pharmaceuticals Inc. Pyrimidinyl sulfonamide compounds which inhibit leukocyte adhesion mediated by vla-4
MX2011011326A (en) * 2009-04-27 2012-02-13 Elan Pharm Inc Pyridinone antagonists of alpha-4 integrins.
US20120258093A1 (en) 2009-08-20 2012-10-11 Institut National De La Sante Et De La Recherche Medicale (Inserm) Vla-4 as a biomarker for prognosis and target for therapy in duchenne muscular dystrophy
BR112018075992A2 (en) 2016-06-13 2019-04-02 Cancer Research Tech Ltd pyridines substituted as dnmt1 inhibitors
US10610104B2 (en) 2016-12-07 2020-04-07 Progenity, Inc. Gastrointestinal tract detection methods, devices and systems
CA3045931A1 (en) 2016-12-14 2018-06-21 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
US20230033021A1 (en) 2018-06-20 2023-02-02 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
AU2019373242B2 (en) 2018-10-30 2023-07-13 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
AU2019373245C1 (en) 2018-10-30 2022-10-27 Gilead Sciences, Inc. Compounds for inhibition of alpha 4β7 integrin
JP7214882B2 (en) 2018-10-30 2023-01-30 ギリアード サイエンシーズ， インコーポレイテッド Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
CN112969687A (en) 2018-10-30 2021-06-15 吉利德科学公司 Quinoline derivatives as alpha 4 beta 7 integrin inhibitors
WO2020106750A1 (en) 2018-11-19 2020-05-28 Progenity, Inc. Methods and devices for treating a disease with biotherapeutics
KR20220047323A (en) 2019-08-14 2022-04-15 길리애드 사이언시즈, 인코포레이티드 Compounds for Inhibiting Alpha 4 Beta 7 Integrin
CN115666704A (en) 2019-12-13 2023-01-31 比奥拉治疗股份有限公司 Ingestible device for delivery of therapeutic agents to the gastrointestinal tract
EP4284947A1 (en) 2021-01-29 2023-12-06 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods of assessing the risk of developing progressive multifocal leukoencephalopathy in patients treated with vla-4 antagonists

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US5510332A (en) 1994-07-07 1996-04-23 Texas Biotechnology Corporation Process to inhibit binding of the integrin α4 62 1 to VCAM-1 or fibronectin and linear peptides therefor
DE69530392D1 (en) 1994-07-11 2003-05-22 Athena Neurosciences Inc INHIBITORS OF LEUKOCYTE ADHESION
US6410729B1 (en) * 1996-12-05 2002-06-25 Amgen Inc. Substituted pyrimidine compounds and methods of use
FR2766183B1 (en) * 1997-07-17 1999-08-27 Rhone Poulenc Rorer Sa MEDICINES CONTAINING NEW POLYHYDROXYBUTYLPYRAZINES, NEW POLYHYDROXYBUTYLPYRAZINES AND THEIR PREPARATION
US6011038A (en) * 1997-09-05 2000-01-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
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Also Published As

Publication number Publication date
US6794506B2 (en) 2004-09-21
US20080182850A1 (en) 2008-07-31
AU2001277960A1 (en) 2002-02-05
US7365073B2 (en) 2008-04-29
WO2002008203A2 (en) 2002-01-31
US20040266763A1 (en) 2004-12-30
US20020052375A1 (en) 2002-05-02

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